Maglitin

MAGLITIN (100 mg): A round shaped, beige film-coated tablet, imprinted with M-H on one side and 2II on the other side.
Each 1 film coated tablet contains sitagliptin phosphate equivalent to sitagliptin 100 mg.

Pharmacology: Pharmacodynamics: MAGLITIN (Sitagliptin phosphate) is an orally-active, potent, and highly selective inhibitor of the dipeptidyl peptidase 4 (DPP-4) enzyme for the treatment of type 2 diabetes. The DPP-4 inhibitors are a class of agents that act as incretin enhancers. By inhibiting the DPP-4 enzyme, sitagliptin increases the levels of two known active incretin hormones, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells, GLP-1 also lowers glucagon secretion from pancreatic alpha cells, leading to reduced hepatic glucose production.
Pharmacokinetics: Absorption: The absolute bioavailability of sitagliptin is approximately 87%, since co-administration of a high-fat meal with MAGLITIN had no effect on the pharmacokinetics.
Distribution: The mean volume of distribution at steady state is approximately 198 liters. The fraction of sitagliptin reversibly bound to plasma proteins is low (38%).
Metabolism: Sitagliptin is primarily eliminated unchanged in urine, and metabolism is a minor pathway. Approximately 79% of sitagliptin is excreted unchanged in the urine. The primary enzyme responsible for the limited metabolism of sitagliptin was CYP3A4, with contribution from CYP2C8.
Elimination: Elimination of sitagliptin occurs primarily via renal excretion. Excretion is mainly via urine 87% (79% as unchanged drug, 16% as metabolite); feces 13%.

Monotherapy: MAGLITIN is indicated as an adjunct to diet and exercise to improve glycemic control in patients with type 2 diabetes mellitus.
Combination with Metformin: MAGLITIN is indicated in patients with type 2 diabetes mellitus to improve glycemic control in combination with metformin as initial therapy or when the single agent alone, with diet and exercise, does not provide adequate glycemic control.
Combination with a Sulfonylurea: MAGLITIN is indicated in patients with type 2 diabetes mellitus to improve glycemic control in combination with a sulfonylurea when treatment with the single agent alone, with diet and exercise, does not provide adequate glycemic control.
Combination with a PPARγ agonist: MAGLITIN is indicated in patients with type 2 diabetes mellitus to improve glycemic control in combination with a PPARγ agonist (i.e., thiazolidinediones) as initial therapy or when the single agent alone, with diet and exercise, does not provide adequate glycemic control.
Combination with Metformin and a Sulfonylurea: MAGLITIN is indicated in patients with type 2 diabetes mellitus to improve glycemic control in combination with metformin and a sulfonylurea when dual therapy with these agents, with diet and exercise, does not provide adequate glycemic control.
Combination with Metformin and a PPARγ agonist: MAGLITIN is indicated in patients with type 2 diabetes mellitus to improve glycemic control in combination with metformin and a PPARγ agonist (i.e., thiazolidinediones) when dual therapy with these agents, with diet and exercise, does not provide adequate glycemic control.
Combination with Insulin: MAGLITIN is indicated in patients with type 2 diabetes mellitus as an adjunct to diet and exercise to improve glycemic control in combination with insulin (with or without metformin).

Recommended Dose/Mode of Administration: The recommended dose of MAGLITIN is 100 mg once daily as monotherapy or as combination therapy with metformin, a sulfonylurea, insulin (with or without metformin), a PPARγ agonist (i.e., thiazolidinediones), metformin plus a sulfonylurea, or metformin plus a PPARγ agonist.
MAGLITIN can be taken with or without food.
When MAGLITIN is used in combination with a sulfonylurea or with insulin, a lower dose of sulfonylurea or insulin may be considered to reduce the risk of sulfonylurea or insulin-induced hypoglycemia (See Hypoglycemia in Combination with a Sulfonylurea or with Insulin under Precautions).
Patients with Renal Impairment: Because there is a dosage adjustment based upon renal function, assessment of renal function is recommended prior to initiation of MAGLITIN and periodically thereafter.
For patients with mild renal impairment (estimated glomerular filtration rate [eGFR] ≥60 to <90 mL/min/1.73 m²), no dosage adjustment for MAGLITIN is required.
For patients with moderate renal impairment (eGFR ≥45 to <60 mL/min/1.73 m²), no dosage adjustment for MAGLITIN is required.
For patients with moderate renal impairment (eGFR ≥30 to <45 mL/min/1.73 m²), the dose of MAGLITIN is 50 mg once daily.
For patients with severe renal impairment (eGFR ≥15 to <30 mL/min/1.73 m²) or with end-stage renal disease (ESRD) (eGFR <15 mL/min/1.73 m²), including those requiring hemodialysis or peritoneal dialysis, the dose of MAGLITIN is 25 mg once daily. MAGLITIN may be administered without regard to the timing of dialysis.

In the event of an overdose, it is reasonable to employ the usual supportive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy if required.

MAGLITIN is contraindicated in patients who are hypersensitivity to any components of this product.

Based on the Ministry of public Health Announcement: 1. Do not use in patients with known hypersensitivity to this medicine.
2. Do not use in type 1 diabetes treatment, patients with ketoacidosis, severe infection or serious accident.
3. Avoid to use in pregnancy and lactation.
4. Should not use concomitantly with alcohol.
5. This drug may increase risk of severe joint pain.

General: MAGLITIN should not be used in patients with type 1 diabetes or for the treatment of diabetic ketoacidosis.
Pancreatitis: There have been reports of acute pancreatitis, including fatal and non-fatal hemorrhagic or necrotizing pancreatitis. If pancreatitis is suspected, MAGLITIN and other potentially suspect medicinal products should be discontinued.
Use in Patients with Renal Impairment: MAGLITIN is renally excreted. To achieve plasma concentrations of MAGLITIN similar to those in patients with normal renal function, lower dosages are recommended in patients with eGFR <45 mL/min/1.73 m², as well as in ESRD patients requiring hemodialysis or peritoneal dialysis.
Hypoglycemia in Combination with a Sulfonylurea or with Insulin: To reduce the risk of sulfonylurea-or insulin-induced hypoglycemia, a lower dose of sulfonylurea or insulin may be considered.
Hypersensitivity Reactions: These reactions include anaphylaxis, angioedema, and exfoliative skin conditions including Stevens-Johnson syndrome. Onset of these reactions occurred within the first 3 months after initiation of treatment with MAGLITIN, with some reports occurring after the first dose. If a hypersensitivity reaction is suspected, discontinue MAGLITIN, assess for other potential causes for the event, and institute alternative treatment for diabetes.
Bullous Pemphigoid: If bullous pemphigoid is suspected, MAGLITIN should be discontinued and referral to a dermatologist should be considered for diagnosis and appropriate treatment.

Pregnancy and Lactation: US FDA category: B.
There are no adequate and well-controlled studies in pregnant women; therefore, the safety of MAGLITIN in pregnant women is not known. MAGLITIN, like other oral antihyperglycemic agents, is not recommended for use in pregnancy. It is not known whether the drug is distributed into human milk. Therefore, MAGLITIN should not be used by women who are nursing.

Endocrine & Metabolic: Hypoglycemia.
Gastrointestinal: Diarrhea, nausea.
Renal: Increased serum creatinine.
Respiratory: Nasopharyngitis, upper respiratory tract infection.

Patients receiving digoxin should be monitored appropriately. No dosage adjustment of digoxin or MAGLITIN is recommended. No dosage adjustment for MAGLITIN is recommended when co-administered with cyclosporine or other p-glycoprotein inhibitors (e.g., ketoconazole).

Store below 30°C.

Antidiabetic Agents

A10BH01 - sitagliptin ; Belongs to the class of dipeptidyl peptidase 4 (DPP-4) inhibitors. Used in the treatment of diabetes.

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